AZD5363

  • CAS: 1143532-39-1
  • MDL:
  • Product number:QC-11881
  • Molecular formula: C21H25ClN6O2
  • Purity: 98.3%
  • MW: 428.92
Size Price Stock
50mg $350 in stock
100mg $595 in stock
250mg $995 in stock
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Brief Description

AZD5363, a novel pyrrolopyrimidine-derived compound, inhibits all AKT isoforms (IC50 <10 nM).
IC50 Value: <10 nM(Akt1/2/3)
Target: pan-Akt
AZD5363 has potential to treat a range of solid and hematologic tumors as monotherapy or a combinatorial agent, and has potential for personalized medicine based on the genetic status of PIK3CA, PTEN, and RAS. in vitro: AZD5363, a novel pyrrolopyrimidine-derived compound, inhibited all AKT isoforms with a potency of 10 nmol/L or less and inhibited phosphorylation of AKT substrates in cells with a potency of approximately 0.3 to 0.8 μmol/L. AZD5363 monotherapy inhibited the proliferation of 41 of 182 solid and hematologic tumor cell lines with a potency of 3 μmol/L or less[1].
in vivo: Oral dosing of AZD5363 to nude mice caused dose- and time-dependent reduction of PRAS40, GSK3β, and S6 phosphorylation in BT474c xenografts (PRAS40 phosphorylation EC(50) ~ 0.1 μmol/L total plasma exposure), reversible increases in blood glucose concentrations, and dose-dependent decreases in 2[18F]fluoro-2-deoxy-D-glucose ((18)F-FDG) uptake in U87-MG xenografts. This compound demonstrated good preclinical drug metabolism and pharmacokinetics (DMPK) properties and, after oral dosing, showed pharmacodynamic knockdown of phosphorylation of Akt and downstream biomarkers in vivo, and inhibition of tumor growth in a breast cancer xenograft model.[1]
Clinical trail: AZD5363 has potential to treat a range of solid and hematologic tumors as monotherapy or a combinatorial agent, AZD5363 is currently in phase I clinical trials.
References on AZD5363:
[1]. Davies BR, Greenwood H, Dudley P, Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background. Mol Cancer Ther. 2012 Apr;11(4):83-87.

Solubility

DMSO 86 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

White to off-white solid

All CEG Chemical products are intended for laboratory research use only.

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